GLYCERYL OLIGONUCLEOTIDE
PURPOSE: To obtain a new compound, a specific glyceryl oligonucleotide, useful as an anti-HIV agent having excellent anti-HIV activity and improved stability in blood by partially substituting deoxyribose with glycerol. CONSTITUTION: This glyceryl oligonucleotide is shown by formula I [DBB is 3,4-(d...
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Zusammenfassung: | PURPOSE: To obtain a new compound, a specific glyceryl oligonucleotide, useful as an anti-HIV agent having excellent anti-HIV activity and improved stability in blood by partially substituting deoxyribose with glycerol. CONSTITUTION: This glyceryl oligonucleotide is shown by formula I [DBB is 3,4-(dibenzyloxy)benzyl; R is guanin-9-yl or adenin-9-yl; R is adenin-9-yl, guanin-9-yl, cytosin-1-yl, thymin-1-yl or uracil-1-yl; (m) is integer of 0 or 1-6; (n) is an integer of 1-6; m+n is 2-10], has excellent anti-HIV activity and improved stability in blood). The compound is obtained by introducing a nucleic acid base into a protected glycerol of formula II, reacting the resultant substance with 4,4'-dimethoxytrityl chloride, reacting the resulting substance with succinic anhydride to give a compound of formula III (R is a nucleic acid base; DMT is 4,4'-dimethoxytrityl), subjecting the compound to extension reaction by phosphoamidite method and deprotecting. |
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